Novel zwitterionic ABA-type triblock copolymer for pH- and salt-controlled release of risperidone

摘要

An ABA-type triblock copolymer was synthesized through group-transfer polymerization by using poly[2(diethylamino) ethyl methacrylate] (PDEA) as A block and poly[2-(dimethylamino) ethyl methacrylate] (PDMA) as B block. By utilizing the 1,3-propane sultone to obtain polyzwitterionic triblock copolymer under moderate conditions, PDMA block of the triblock copolymer has been selectively betainized. The selectively betainized block copolymer and its precursor were molecularly dissolved in acidic aqueous media without any use of cosolvent at room temperature. In both cases, an increase in solution pH caused near monodisperse cationic or neutral flower-like micellization with hydrophobic PDEA-core at basic aqueous solution. However, at higher polymer concentrations where precursor triblock copolymer does not exhibit any gelling behavior (10% and higher), polyzwitterionic copolymer derivative can be gelated as a result of inter-chain integration of polyzwitterionic groups. Furthermore, the load of risperidone (RISP) into gel matrix and release studies have been successively realized. The results indicated that the betainized novel gel is appropriate for using as a pH- and salt-controlled risperidone-releasing system.